1-oxa-5-aza-bicyclo (4.2.0) Octanes (including Unsaturated) Patents (Class 514/210.08)
  • Patent number: 8592454
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
  • Patent number: 8569281
    Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: October 29, 2013
    Assignees: Medical Research Council Technology, Genentech, Inc.
    Inventors: Bryan K. Chan, Huifen Chen, Anthony Estrada, Daniel Shore, Zachary Sweeney, Edward Giles McIver
  • Patent number: 8529935
    Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: September 10, 2013
    Assignees: Mero S.R.L., Novagenit S.R.L.
    Inventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
  • Publication number: 20130131032
    Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 23, 2013
    Applicant: Revaax Pharmaceuticals, LLC
    Inventor: Revaax Pharmaceuticals, LLC
  • Publication number: 20130102583
    Abstract: A compound of the formula: wherein X is —N?, —CH?, or the like; W is —CH2— or the like; U is —S— or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3 is hydrogen or the like; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is —C(?O)—, or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: April 4, 2011
    Publication date: April 25, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Shinya Hisakawa, Yasushi Hasegawa, Toshiaki Aoki, Hiroki Kusano, Masayuki Sano, Jun Sato, Kenji Yamawaki
  • Publication number: 20120172292
    Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 5, 2012
    Applicant: NEW YORK UNIVERSITY
    Inventors: Evgeny A. Nudler, Ivan Gusarov
  • Publication number: 20110294774
    Abstract: The present invention provides a pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, an antibacterially effective combination of a ?-lactam antibiotic and an inhibitor of any bacterial peptidoglycan biosynthesis enzyme, especially GlmU, GlmU, MurA, MurB, MurC, MurD, MurE, MurF, MurG, MraY, and UppS.
    Type: Application
    Filed: May 6, 2011
    Publication date: December 1, 2011
    Applicant: TRIUS THERAPEUTICS
    Inventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
  • Publication number: 20110280921
    Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 17, 2011
    Applicants: NOVAGENIT S.R.L., MERO S.R.L
    Inventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
  • Publication number: 20110257147
    Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Applicant: Revaax Pharmaceuticals, LLC
    Inventor: Gary A. Koppel
  • Publication number: 20110046101
    Abstract: The present invention relates to broad spectrum ?-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) ?-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I) wherein R1 is selected from R2 is selected from with certain provisos as herein defined; in combination with a pharmaceutically acceptable ?-lactam antibiotic in an amount which is effective for treating the bacterial infection.
    Type: Application
    Filed: March 17, 2008
    Publication date: February 24, 2011
    Inventors: Gary I. Dmitrienko, Jarrod W. Johnson, Timothy R. Ramadhar, Thammaiah Viswanatha, Sundaramma Viswanatha
  • Patent number: 7842683
    Abstract: Administration of ?-Lactam compounds, including ?-lactam antibiotics and ?-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.
    Type: Grant
    Filed: January 23, 2008
    Date of Patent: November 30, 2010
    Assignee: Revaax Pharmaceuticals, LLC
    Inventor: Gary A. Koppel
  • Publication number: 20100249090
    Abstract: Neurotherapeutically effective pharmaceutical compositions are described that include carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are ?-lactam compounds, particularly penam and cephem ?-lactam antibiotics and non-antibiotic derivatives thereof.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 30, 2010
    Inventors: Gary A. Koppel, Michael O. Chaney
  • Publication number: 20100040548
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: June 10, 2009
    Publication date: February 18, 2010
    Inventor: Chongxi Yu
  • Publication number: 20090253676
    Abstract: Compounds of Formula (I): wherein: R1 is hydroxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.
    Type: Application
    Filed: December 16, 2008
    Publication date: October 8, 2009
    Applicant: AstraZeneca AB
    Inventors: Craig Johnstone, Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Publication number: 20080312203
    Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: August 21, 2008
    Publication date: December 18, 2008
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Patent number: 7439253
    Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: October 21, 2008
    Assignee: Novexel
    Inventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
  • Publication number: 20080200447
    Abstract: Administration of ?-Lactam compounds, including ?-lactam antibiotics and ?-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.
    Type: Application
    Filed: January 23, 2008
    Publication date: August 21, 2008
    Applicant: REVAAX PHARMACEUTICALS, LLC
    Inventor: Gary A. Koppel
  • Publication number: 20080146535
    Abstract: The present invention relates to pharmaceutical compositions of carbocephem antibiotics with ?-lactamase inhibitors useful for the treatment of bacterial infections, in particular infections caused by bacteria that express ?-lactamases as a mechanism of resistance to ?-lactam antibiotics.
    Type: Application
    Filed: September 2, 2005
    Publication date: June 19, 2008
    Inventors: Tomasz Glinka, George Miller
  • Patent number: 6627625
    Abstract: Administration of &bgr;-lactam compounds including &bgr;-lactam antibiotics and &bgr;-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.
    Type: Grant
    Filed: August 16, 2000
    Date of Patent: September 30, 2003
    Assignee: Revaax Pharmaceuticals, LLC
    Inventor: Gary A. Koppel
  • Patent number: 6514962
    Abstract: Stabilized preparations which contain a &bgr;-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
    Type: Grant
    Filed: February 5, 2001
    Date of Patent: February 4, 2003
    Assignee: Takeda Schering-Plough Animal Health K.K.
    Inventors: Hatsuo Shibatani, Tomoyasu Nakamura
  • Patent number: 6489319
    Abstract: Administration of inhibitors of carboxypeptidase E provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition. Certain &bgr;-Lactam antibiotics, most significantly, certain 1-oxa-1-dethia cephems with blood brain barrier transport, exhibit potent therapeutic neurologic activity.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: December 3, 2002
    Assignee: Revaax Pharmaceuticals, LLC
    Inventors: Gary A. Koppel, Michael O. Chaney
  • Patent number: 6475522
    Abstract: Synthetic polymer compositions contain antibiotics as antidegradants. Antibiotics from classes of glycopeptides and &bgr;-lactams have been found to prevent or inhibit synthetic polymer degradation.
    Type: Grant
    Filed: August 30, 2000
    Date of Patent: November 5, 2002
    Assignee: Hammond Group, Inc.
    Inventor: Richard F. Grossman